2. Metabolic Enzyme/Protease Autophagy
  3. FXR Autophagy
  4. Nidufexor

Nidufexor (LMB763) is an orally-available farnesoid X receptor (FXR) agonist for the research of nonalcoholic steatohepatitis (NASH).

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Nidufexor

Nidufexor 화학구조

CAS No. : 1773489-72-7

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무료 샘플 (0.1 - 0.2 mg)   지금 신청하기  
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
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Solution
10 mM * 1 mL in DMSO 해외재고보유
Solid
5 mg 해외재고보유
10 mg 해외재고보유
25 mg 해외재고보유
50 mg 해외재고보유
100 mg 해외재고보유
200 mg   견적 받기  
500 mg   견적 받기  

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제품 설명

Nidufexor (LMB763) is an orally-available farnesoid X receptor (FXR) agonist for the research of nonalcoholic steatohepatitis (NASH)[1].

IC50 & Target

FXR[1]
Cellular Effect
Cell Line Type Value Description References
Jurkat EC50
> 80 μM
Compound: 1; LMB763
Agonist activity at human GPBAR1 expressed in Jurkat cells assessed as increase in intracellular cAMP level incubated for 1 hr by fluorescence based assay
Agonist activity at human GPBAR1 expressed in Jurkat cells assessed as increase in intracellular cAMP level incubated for 1 hr by fluorescence based assay
[PMID: 31940200]
In Vivo

Nidufexor (LMB763) is a potent and specific FXR-gene modulator in vivo, reducing steatosis, inflammation and fibrosis in nonalcoholic steatohepatitis (NASH) murine models[1].
? Nidufexor exhibits moderate Cmax (4.5, 12.4, 28.1, 80.9, and 140.8 μM) and terminal elimination half-lives (t1/2; 3.9 5.7 6.3 5.6 6.3 h) following oral administration (3 ,10 ,30, 100, and 300mg/kg) in adult male Wistar Han rats (age approximately 10 weeks)[1]
? Nidufexor exhibits terminal elimination half-lives (mouse 4.5, rat 4.4 and, dog 6.8 h) following intravenous administration (mouse 3.0, rat 5.0 and, dog 0.5 mg/kg)[1].
? Nidufexor exhibits terminal elimination half-lives (mouse 3.5, rat 2.7 and, dog 10.1 h) following oral administration (mouse 10, rat 10 and, dog 2 mg/kg)[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Han-Wistar rats[1]
Dosage: 0.1, 0.3, 1.5, 7.5, 25, 100 mg/kg (Pharmacokinetic Analysis)
Administration: Oral gavage, once daily for 14 days
Result: On day 1 and 13, serum exposure increased approximately dose-proportionally from 0.1 to 100 mg/kg. Exposure at 0.1 and 0.3 mg/kg was likely underestimated on day 13. No significant accumulation was observed[1].
Clinical Trial
분자량

487.93

화학식

C27H22ClN3O4
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

CN1C(C2=CC(Cl)=CC=C2OC3)=C3C(C(N(CC4=CC=CC=C4)CC5=CC=C(C(O)=O)C=C5)=O)=N1
선적

Room temperature in continental US; may vary elsewhere.
보관
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
용액&용해도
In Vitro: 

DMSO : 83.33 mg/mL (170.78 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.0495 mL 10.2474 mL 20.4947 mL
5 mM 0.4099 mL 2.0495 mL 4.0989 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • 몰농도 계산기

  • 농도 희석 계산기

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.08 mg/mL (4.26 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% Corn Oil

    Solubility: ≥ 2.08 mg/mL (4.26 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
순도&문서

Purity: 99.67%

SDS (393 KB)

COA (250 KB) RP-HPLC (250 KB) MS (68 KB)

Handling Instructions (2659 KB)
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.0495 mL 10.2474 mL 20.4947 mL 51.2369 mL
5 mM 0.4099 mL 2.0495 mL 4.0989 mL 10.2474 mL
10 mM 0.2049 mL 1.0247 mL 2.0495 mL 5.1237 mL
15 mM 0.1366 mL 0.6832 mL 1.3663 mL 3.4158 mL
20 mM 0.1025 mL 0.5124 mL 1.0247 mL 2.5618 mL
25 mM 0.0820 mL 0.4099 mL 0.8198 mL 2.0495 mL
30 mM 0.0683 mL 0.3416 mL 0.6832 mL 1.7079 mL
40 mM 0.0512 mL 0.2562 mL 0.5124 mL 1.2809 mL
50 mM 0.0410 mL 0.2049 mL 0.4099 mL 1.0247 mL
60 mM 0.0342 mL 0.1708 mL 0.3416 mL 0.8539 mL
80 mM 0.0256 mL 0.1281 mL 0.2562 mL 0.6405 mL
100 mM 0.0205 mL 0.1025 mL 0.2049 mL 0.5124 mL
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Nidufexor Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Nidufexor1773489-72-7LMB763LMB 763LMB-763FXRAutophagyNR1H4Inhibitorinhibitorinhibit

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상품명:
Nidufexor
Cat. No.:
HY-109096
수량:
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